A series of small-molecule inhibitors targeting FTO have been developed demonstrating promising therapeutic activity across several diseases, including AML, clear cell renal cell carcinoma, nasopharyngeal carcinoma, hepatocarcinoma, breast cancer, glioblastoma, glioma, esophageal cancer, melanoma, gastric cancer, uterine leiomyosarcoma, obesity, epilepsy, Alzheimer’s disease, pancreatitis and diabetes (Table 3) [31, 95–122]. Here, FTO is linked to breast cancer.